Development and evaluation of febuxostat solid dispersion through screening method
Febuxostat (Febux) is a BCS II drug and has a very low solubility. In order to overcome this shortcoming, the purpose of study is to increase the in vitro dissolution (%) and drug release (%) of Febux by using a screening method. The Febux-SD formulation was prepared by screening solubilizers, pH agents, and carriers using with a solvent evaporation method.
The novel Febux SD formulation was successfully developed. The dissolution (%) of Febux of optimal formulation (SD3) was higher than that of Feburic® tab in pH 1.2, distilled water (DW), and pH6.8 buffer by 6.3-, 2.5-, and 1.1-fold, respectively, at 60 min. The in vitro drug release (%) and permeability (μg/cm2) of SD3 formulation were improved compared to those of Feburic® tab in the pH shifting method and PBS (7.4), respectively. The SD3 formulation was well maintained the stability for 6 months, and that of physicochemical properties were altered. In conclusion, the Febux solubilization study with meglumine was first attempted and successfully performed. Through the improved dissolution (%) of Febux, high bioavailability of SD3 formulation is expected in animal and human studies.
2.1. Materials
Febuxostat (Febux), meglumine, MgO, PVP/VA S-630, and Neusilin® (US2 and UFL2) were provided by Yuyu Pharma Inc. (Korea, Suwon-si). Sodium oleate (extra pure) was purchased from Junsei Chemical Co. Ltd. (Tokyo, Japan). Sodium hydroxide was purchased from Daejung Chemicals & Metals Co. LTD (Siheung, Korea). Kolliphor® (P188 and P407), PEG6000, Kollicoat® (IR), Kollidon® (K12, K17, K30, and K90), Kolliphor® (HS 15), Soluplus®, and TPGS were obtained from BASF (Ludwigshafen, Germany). Fumed silica Aerosil® (200 and 300) were provided by Evonik (Essen, Germany). Mannitol, lactose, microcrystalline cellulose, granular dicalcium phosphate anhydrate (DCP-A), and granular dicalcium phosphate dihydrate (DCP-D) were obtained from Whawon Pharm (Seoul, Korea). Sodium carbonate anhydrous, sodium bicarbonate, potassium hydroxide, sodium phosphate dibasic anhydrous, ethyl alcohol, and universal buffers were purchased from Samchun Pure Chemical Co., Ltd. (Pyeongtaek, Korea).
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Jeong Sun Sohn, Jin-Seok Choi, Development and evaluation of febuxostat solid dispersion through screening method, Saudi Pharmaceutical Journal, 2023, 101724, ISSN 1319-0164,
https://doi.org/10.1016/j.jsps.2023.101724.